Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T25307 | Target Info | |||
| Target Name | Nuclear receptor ROR-gamma (RORG) | ||||
| Synonyms |
Retinoid-related orphan receptor-gamma; RZRG; RORG; RAR-related orphan receptor C; Nuclear receptor subfamily 1 group F member 3; Nuclear receptor RZR-gamma; NR1F3
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| Target Type | Clinical trial Target | ||||
| Gene Name | RORC | ||||
| Biochemical Class | Nuclear hormone receptor | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 21 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-(1,3-Benzodioxol-5-yl)-N,N-diethyl-3-(2-hydroxy-4,6-dimethoxyphenyl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
MLS000879443; CHEMBL1445011; KUC101573N; SCHEMBL14826357; HMS2220L21; HMS3341O16; BDBM50426383; NCGC00166470-01; NCGC00238440-01; SMR000465495
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4211299
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Investigative | Compound Info | ||
| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
3-(1,3-Benzodioxol-5-yl)-3-(2-hydroxy-4,6-dimethoxyphenyl)-N-(4-methylphenyl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2326699; SCHEMBL14826344; BDBM50426381; NCGC00189210-01
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
3-(1,3-Benzodioxol-5-yl)-3-(2-hydroxy-4,6-dimethoxyphenyl)-1-pyrrolidin-1-ylpropan-1-one
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Investigative | Compound Info | ||
| Synonyms |
MLS000879447; CHEMBL1879167; KUC101568N; SCHEMBL14826354; HMS2220N23; HMS3339L22; BDBM50426386; NCGC00166469-01; NCGC00238438-01; SMR000465494
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
N-(1-Acetyl-2,3-dihydroindol-5-yl)-1-ethyl-2-oxobenzo[cd]indole-6-sulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3234033; SCHEMBL16862779; BDBM50005513
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| Activity |
IC50 = 52260 nM
|
[3] | |||
| Compound Name |
2-({4-Allyl-5-[(4-chlorophenoxy)methyl]-4H-1,2,4-triazol-3-yl}sulfanyl)-N'-(3-hydroxybenzylidene)acetohydrazide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3210331; SMR000162176; MLS000546137; BDBM50005519; STK958813; AKOS005677873; AK-968/15254261
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| Activity |
IC50 = 56640 nM
|
[3] | |||
| Compound Name |
N-(2,4-Difluorophenyl)-2-[N-(4-methylphenyl)sulfonyl-3-(trifluoromethyl)anilino]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3797260; ZINC1126032; BDBM50164887; MCULE-4485073875
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| Activity |
IC50 = 62580 nM
|
[4] | |||
| Compound Name |
2-(4-Cyano-N-(4-methylphenyl)sulfonylanilino)-N-(4-cyanophenyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3798333; BDBM50165109
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| Activity |
IC50 = 65320 nM
|
[4] | |||
| Compound Name |
Methyl 4-[[[2-[N-(4-methylphenyl)sulfonyl-3-(trifluoromethyl)anilino]acetyl]amino]methyl]benzoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3799245; BDBM50165075
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| Activity |
IC50 = 67050 nM
|
[4] | |||
| Compound Name |
Chembl4176087
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Investigative | Compound Info | ||
| Synonyms |
BDBM50281851
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| Activity |
IC50 = 69000 nM
|
[5] | |||
| Compound Name |
N-(4-Acetylphenyl)-1-ethyl-2-oxobenzo[cd]indole-6-sulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3234251; SCHEMBL16866204; BDBM50005481
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|
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| Activity |
IC50 = 70140 nM
|
[3] | |||
| Compound Name |
5-[(2-Chlorophenoxy)methyl]-N-(4-sulfamoylphenyl)furan-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3234273; N-[4-(aminosulfonyl)phenyl]-5-[(2-chlorophenoxy)methyl]-2-furamide; ZINC2763584; BDBM50005531; STK966009; AKOS001693082; MCULE-8511453977; EU-0016667; AK-968/40709644; SR-01000113753; SR-01000113753-1
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| Activity |
IC50 = 81690 nM
|
[3] | |||
| Compound Name |
N-(4-(1-Ethyl-2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamido)phenyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3234256; Oprea1_792252; Oprea1_827954; SCHEMBL16862777; ZINC1448661; BDBM50005485; AKOS000808041; MCULE-6625831404; ST50072658; AQ-390/40910485; SR-01000082854; SR-01000082854-1; F1094-0299; N-[4-[(1-ethyl-2-oxobenzo[cd]indol-6-yl)sulfonylamino]phenyl]acetamide
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| Activity |
IC50 = 89760 nM
|
[3] | |||
| Compound Name |
N-[(4-Methylphenyl)sulfonyl]-N-[3-(trifluoromethyl)phenyl]glycine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3798394; ALBB-029343; ZINC5600859; 2-[N-(4-methylphenyl)sulfonyl-3-(trifluoromethyl)anilino]acetic acid; BBL019693; BDBM50164889; MFCD02636370; STL222156; AKOS000297529; MCULE-7667177021; VS-06960; ST51015354; AB00104459-01; SR-01000230825; SR-01000230825-1; 2-{[(4-methylphenyl)sulfonyl][3-(trifluoromethyl)phenyl]amino}acetic acid; 2-{N-[3-(trifluoromethyl)phenyl]4-methylbenzenesulfonamido}acetic acid; glycine, N-[(4-methylphenyl)sulfonyl]-N-[3-(trifluoromethyl)phenyl]-
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| Activity |
IC50 = 93290 nM
|
[4] | |||
| Compound Name |
2-[N-(4-Methylphenyl)sulfonyl-3-(trifluoromethyl)anilino]-N-(4-phenylmethoxyphenyl)acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3797861; BDBM50164891; ZINC108882029
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|
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| Activity |
IC50 = 93850 nM
|
[4] | |||
| Compound Name |
N-[4-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl]-2-[N-(4-methylphenyl)sulfonyl-3-(trifluoromethyl)anilino]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3799700; BDBM50165107
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| Activity |
IC50 = 112250 nM
|
[4] | |||
| Compound Name |
2-({5-[3-(1,3-Dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)propyl]-4-(prop-2-en-1-yl)-4H-1,2,4-triazol-3-yl}sulfanyl)-N-(4-sulfamoylphenyl)acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3234278; ZINC8433335; BDBM50005545; STL444010; AKOS001057969; MCULE-7421078081; ST50055977
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| Activity |
IC50 = 142210 nM
|
[3] | |||
| Compound Name |
N-(2-Benzoylphenyl)-1-ethyl-2-oxobenzo[cd]indole-6-sulfonamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3234245; SCHEMBL16862807; BDBM50005515
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|
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| Activity |
IC50 = 156300 nM
|
[3] | |||
| Compound Name |
N-(4-Carbamoylphenyl)-3-[(4-chlorophenoxy)methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3234272; ZINC2762368; BDBM50005529; STK316538; AKOS003793622; MCULE-3353974089
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| Activity |
IC50 = 168270 nM
|
[3] | |||
| Compound Name |
1-Ethyl-N-[(4-methoxyphenyl)methyl]-2-oxobenzo[cd]indole-6-sulfonamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3234260; SCHEMBL16866280; BDBM50005517
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|
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| Activity |
IC50 = 174400 nM
|
[3] | |||
| Compound Name |
N-[2-(4-Acetylpiperazin-1-yl)-2-oxoethyl]-4-methyl-N-[3-(trifluoromethyl)phenyl]benzenesulfonamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3797484; BDBM50164893
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|
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| Activity |
IC50 = 175300 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4166708
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50282112; EE8
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|
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| Activity |
IC50 = 216000 nM
|
[5] | |||
| Compound Name |
Chembl4171447
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|
Investigative | Compound Info | ||
| Synonyms |
SCHEMBL16799135; 2-(4-ethylsulfonylphenyl)acetamide; BDBM50281914; 2-(4-(ethylsulfonyl)phenyl)acetamide; 2-[4-(ethanesulfonyl)phenyl]acetamide
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| Activity |
IC50 > 500000 nM
|
[5] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification of Potent and Selective Diphenylpropanamide ROR Inhibitors. ACS Med Chem Lett. 2013 Jan 10;4(1):79-84. | ||||
| REF 2 | Design, synthesis and phenotypic evaluation of N-biaryl amides for IL-17A suppression. Medchemcomm. 2016;7:2344-8. | ||||
| REF 3 | Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new ROR inhibitors using virtual screening, synthesis and biological evaluation. Eur J Med Chem. 2014 May 6;78:431-41. | ||||
| REF 4 | Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new ROR inverse agonists: Virtual screening, structure-based optimization, and biological evaluation. Eur J Med Chem. 2016 Jun 30;116:13-26. | ||||
| REF 5 | Optimizing a Weakly Binding Fragment into a Potent RORt Inverse Agonist with Efficacy in an in Vivo Inflammation Model. J Med Chem. 2018 Aug 9;61(15):6724-6735. | ||||
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